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吲哚美辛共聚維酮非晶態(tài)制劑的性質及體外溶出度考察

發(fā)布時間:2018-07-03 16:56

  本文選題:吲哚美辛 + 非晶態(tài) ; 參考:《中國藥學雜志》2017年01期


【摘要】:目的以共聚維酮(Co-PVP)為載體制備吲哚美辛非晶態(tài)制劑,對其加以表征以探討藥物分子與Co-PVP間的相互作用形式,并比較吲哚美辛晶態(tài)與非晶態(tài)的體外溶出差異。方法考察了Co-PVP對吲哚美辛超飽和溶液的結晶抑制作用。采用溶劑蒸發(fā)法制備吲哚美辛非晶態(tài)制劑,通過差示掃描量熱(DSC)、粉末X射線衍射(PXRD)和傅立葉紅外光譜(FTIR)技術對其表征,并進行了體外溶出實驗。結果 Co-PVP對吲哚美辛超飽和溶液有較強的抑晶作用。吲哚美辛與Co-PVP分子之間形成氫鍵,主藥以非晶態(tài)分散于載體中,該非晶態(tài)制劑的體外溶出速率和程度均顯著增加。結論以Co-PVP為載體制備的非晶態(tài)制劑能顯著提高吲哚美辛體外溶出,可為獲得穩(wěn)定的藥物非晶態(tài)制劑提供參考。
[Abstract]:Objective to prepare indomethacin amorphous preparation with co-PVP as carrier, to investigate the interaction between drug molecules and Co-PVP, and to compare the dissolution of indomethacin in vitro. Methods the inhibition of Co-PVP on the crystallization of indomethacin supersaturated solution was investigated. Indomethacin amorphous preparation was prepared by solvent evaporation method. It was characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR). Results Co-PVP had strong inhibitory effect on indomethacin supersaturated solution. The hydrogen bond between indomethacin and Co-PVP was formed, and the main drug was dispersed in the carrier in amorphous state. The dissolution rate and degree of the amorphous preparation in vitro increased significantly. Conclusion Co-PVP as carrier can significantly improve the dissolution of indomethacin in vitro and provide a reference for obtaining stable amorphous preparations.
【作者單位】: 河南大學;天津藥物研究院有限公司釋藥技術與藥代動力學國家重點實驗室;天津中醫(yī)藥大學;
【基金】:國家重大新藥創(chuàng)制項目(2014ZX09507005-002)
【分類號】:R943

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